Santaris Pharma A/S announced the initiation of an open-label, non-randomized Phase 1 study with its HIF-1 alpha antagonist (EZN-2968) licensed outside Europe in 2006 to Enzon Pharmaceuticals, Inc. USA.
The study is designed to evaluate the safety, tolerability, and pharmacokinetics of the HIF-1 alpha anta¬gonist in a daily for 5 days schedule in approximately 30 patients with advanced solid tumors or lymphoma.
“We are very encouraged that Enzon Pharmaceuticals has initiated the second phase 1 study with EZN-2968, a novel RNA-targeted drug based on Santaris Pharmas Locked Nucleic Acid (LNA) technology,” said Keith McCullagh, CEO of Santaris Pharma A/S. “The early safety data on the ongoing cancer trial are encouraging and Enzon is now evaluating alternative dose schedules in this second human study in patients with advanced cancer.”
The investigational drug blocks the production of Hypoxia-inducible factor-1 alpha (HIF-1 alpha), a key regulator of a large number of genes important in cancer biology, including many involved in angio¬genesis, cell proliferation, apoptosis and cell invasion. HIF-1 alpha is low in normal cells, but ele¬vated in a variety of cancers. High expression of HIF-1 alpha is strongly correlated with poor prognosis and re¬sis¬tance to the¬rapy. Therefore, drugs that inhibit HIF-1 alpha are expected to block multiple mechanisms that control cancer progression.